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Updated: Feb 1, 2026

In Vitro Transcription Assays and Their Application in Drug Discovery
Published on: September 20, 2016
A Universal Assay for Aminopeptidase Activity and Its Application for Dipeptidyl Peptidase-4 Drug Discovery
Arkadiy A Bazhin, Marc Chambon, Jonathan Vesin
1Microbiome and Metabolism , Nestlé Institute of Health Sciences SA , Lausanne 1015 , Switzerland.
Abstract:
Aminopeptidases, such as dipeptidyl peptidase-4 (DPP-4, CD26), are potent therapeutic targets for pharmacological interventions because they play key roles in many important pathological pathways. To analyze aminopeptidase activity in vitro (including high-throughput screening [HTS]), in vivo, and ex vivo, we developed a highly sensitive and quantitative bioluminescence-based readout method. We successfully applied this method to screening drugs with potential DPP-4 inhibitory activity. Using this method, we found that cancer drug mitoxantrone possesses significant DPP-4 inhibitory activity both in vitro and in vivo. The pharmacophore of mitoxantrone was further investigated by testing a variety of its structural analogues.
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